Intermediates for the preparation of .DELTA..sup.4,9(11),17(20)
-pregnatriene-3-ones
    3.
    发明授权
    Intermediates for the preparation of .DELTA..sup.4,9(11),17(20) -pregnatriene-3-ones 失效
    制备DELTA 4,9(11),17(20) - 三烯-3-酮的中间体

    公开(公告)号:US5594127A

    公开(公告)日:1997-01-14

    申请号:US557594

    申请日:1995-11-14

    摘要: A compound having a formula ##STR1## in which K is defined as above, C--P being CH.sub.2 or --C.dbd.CH.sub.2 or ##STR2## and J is --SO.sub.2 R.sub.2, or C--P is C.dbd.O and J is --CH.sub.2 Hal.sub.2, or C--P is --CH SO.sub.2 R.sub.2 and J is CO.sub.2 R or Hal.sub.1, R.sub.2 is methyl, phenyl, tolyl or xylyl, R is alkyl of 1 to 6 carbon atoms, aralkyl of 7 to 15 is carbon atoms or a silylated remainder selected from the group consisting of trimethylsilyl, tert.-butyldimethylsilyl, triphenylsilyl and diphenyltert.-butylsilyl, Hal.sub.1 is halogen, Hal.sub.2 is chlorine, bromine or iodine and the wavy lines symbolize any one of the isomer forms or their mixtures which are intermediates.

    摘要翻译: 具有式“IMAGE”G的化合物,其中K如上所定义,CP是CH 2或-C = CH 2或者,而J是-SO 2 R 2,或CP是C = O,J是-CH 2 Hal 2,或CP是 -CH + Z SO 2 R 2,J为+ Z CO 2 R或Hal 1,R 2为甲基,苯基,甲苯基或二甲苯基,R为1至6个碳原子的烷基,7至15的芳烷基为碳原子或选自 由三甲基甲硅烷基,叔丁基二甲基甲硅烷基,三苯基甲硅烷基和二苯基叔丁基甲硅烷基组成,Hal1是卤素,Hal2是氯,溴或碘,波浪线表示任何一种异构体形式或它们作为中间体的混合物。

    Perfumant cyclopropane-carboxylic acid derivatives
    5.
    发明授权
    Perfumant cyclopropane-carboxylic acid derivatives 失效
    香料环丙烷 - 羧酸衍生物

    公开(公告)号:US4431576A

    公开(公告)日:1984-02-14

    申请号:US343348

    申请日:1982-01-27

    摘要: A compound in all its possible isomeric forms and mixtures thereof of the formula ##STR1## wherein R is selected from the group consisting of (a) alkyl of 1 to 12 carbon atoms optionally substituted with cycloalkyl or cycloalkenyl of 3 to 6 carbon atoms or a hydrocarbon chain of 2 to 8 carbon atoms optionally interrupted by an oxygen or ketone, (b) alkenyl and alkynyl of 3 to 8 carbon atoms, (c) cycloalkyl of 3 to 12 carbon atoms optionally containing at least one double bond and substituted with at least one alkyl and (d) aralkyl of 7 to 12 carbon atoms optionally substituted with at least one member of the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen and --CF.sub.3 and R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, --CHO, --COAlK.sub.1, --COOAlK.sub.2 and --CN, at least one being hydrogen, AlK.sub.1 and AlK.sub.2 are alkyl of 1 to 8 carbon atoms and R.sub.1 and R.sub.2 taken together with the carbon atom to which they are attached form the group ##STR2## and X is selected from the group consisting of sulfur, oxygen and imino joined to the 1-carbon atom with a double bond with the proviso that the double bond has the E geometry when R.sub.1 or R.sub.2 are --CHO, --COAlK.sub.1, --COOAlK.sub.2 or ##STR3## and their preparation and odorant compositions containing at least one compound of formula I as a perfume agent.

    摘要翻译: 化合物,其全部可能的异构形式及其混合物,其中R选自(a)任选被3至6个碳原子的环烷基或环烯基取代的1至12个碳原子的烷基或 2至8个碳原子的烃链任选被氧或酮中断,(b)3至8个碳原子的烯基和炔基,(c)3至12个碳原子的环烷基,任选地含有至少一个双键并被 至少一个烷基和(d)7-12个碳原子的芳烷基,任选被至少一个1-4个碳原子的烷基,1-4个碳原子的烷氧基,卤素和-CF 3和R 1和 R2分别选自氢,-CHO,-COAlK1,-COOAlK2和-CN,至少一个为氢,AlK1和AlK2为1至8个碳原子的烷基,R1和R2与碳原子一起 它们所连接的组由和X选自硫,氧和亚氨基与具有双键的1-碳原子连接,条件是当R1或R2为-CHO,-COAlK1, - COOAlK2或及其制备和加味剂组合物,其含有至少一种式I化合物作为预浸剂。

    .beta.-Lactones of 2-hydroxy-cyclopentane-carboxylic acids
    6.
    发明授权
    .beta.-Lactones of 2-hydroxy-cyclopentane-carboxylic acids 失效
    β-内酯2-羟基 - 环戊烷 - 羧酸的内酯

    公开(公告)号:US4308209A

    公开(公告)日:1981-12-29

    申请号:US216124

    申请日:1980-12-15

    摘要: Novel .beta.-lactones of 2-hydroxy-cyclopentane-carboxylic acids of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and methyl and R.sub.2 is selected from the group consisting of --CH.sub.2 --O--CH.sub.2 --CH.sub.3 and --X--Ar, X is selected from the group consisting of --O-- and --CH.sub.2 --, Ar is an optionally substituted member selected from the group consisting of thienyl, thiazolyl, phenyl and thiadiazolyl, the optional substituents being at least one member selected from the group consisting of halogen and --CF.sub.3 and the wavy lines indicate that the groups may be in the .alpha.,.beta. or .beta.,.alpha.-positions or mixtures thereof having hypotensive activity and their preparation.

    摘要翻译: 式(I)的2-羟基 - 环戊烷 - 羧酸的新型β-内酯,其中R 1选自氢和甲基,R 2选自-CH 2 -O-CH 2 -CH 3和 -X-Ar,X选自-O-和-CH 2 - ,Ar是选自噻吩基,噻唑基,苯基和噻二唑基的任选取代的成员,任选的取代基是至少一个选自 由卤素和-CF 3组成的组和波浪线表示这些基团可以是具有低血压活性的α,β或β,α-位或其混合物及其制备。

    Process for the preparation of biphenyl derivatives
    7.
    发明授权
    Process for the preparation of biphenyl derivatives 失效
    联苯衍生物的制备方法

    公开(公告)号:US5618975A

    公开(公告)日:1997-04-08

    申请号:US449396

    申请日:1995-05-24

    摘要: Biphenyl derivatives and processes for the preparation of biphenyl derivatives are described. A compound of formula (I) is disclosed ##STR1## in which the substituent X is --CHO or --CH(OR.sup.1)OR.sup.2, where R.sup.1 and R.sup.2 independently of one another are (C.sub.1 -C.sub.6)-alkyl or R.sup.1 and R.sup.2 together are an alkylene group (--CH.sub.2).sub.n --, where n is 2, 3 4 or 5 and R is --F, --Cl, --NO.sub.2, --(CH.sub.2).sub.m --COOR.sup.3, --(CH.sub.2).sub.m --CONHR.sup.3, --(CH.sub.2).sub.m --CN, --SO.sub.2 NH--COOR.sup.3, --SO.sub.2 NH--CO--NHR.sup.3, --SO.sub.2 NH--SO.sub.2 --R.sup.3, --NHSO.sub.2 R.sup.3, ##STR2## --PO.sub.3 R.sup.3, --NH--SO.sub.2 --CF.sub.3, --SO.sub.2 NR.sup.4 where R.sup.3 is hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.3 -C.sub.6)cycloalkyl, or (C.sub.1 -C.sub.6)-alkyl-(C.sub.3 -C.sub.6)cycloalkyl and R.sup.4 is a group .dbd.C--N(CH.sub.3).sub.2, and m is 0, 1, 2, 3, or 4. The invention also relates to a process for the preparation of a compound of the formula (I) in which X is an optionally protected formyl group and R is a group which is itself inert to the reaction conditions of the synthesis, which comprises reacting a compound of the formula (II) ##STR3## with a substituted phenyl-halogen compound of the formula (III) ##STR4## wherein the substituent Hal is a halogen group.

    摘要翻译: 描述了联苯衍生物和制备联苯衍生物的方法。 公开了式(I)化合物,其中取代基X为-CHO或-CH(OR 1)OR 2,其中R 1和R 2彼此独立地为(C 1 -C 6) - 烷基或R 1和 R2一起是亚烷基(-CH 2)n - ,其中n是2,3,4或5,R是-F,-Cl,-NO 2, - (CH 2)m -COOR 3, - (CH 2)m -CONHR 3, - (CH2)m-CN,-SO2NH-COOR3,-SO2NH-CO-NHR3,-SO2NH-SO2-R3,-NHSO2R3,-PO3R3,-NH-SO2-CF3,-SO2NR4,其中R3是氢, (C 1 -C 6) - 烷基,(C 3 -C 6)环烷基或(C 1 -C 6) - 烷基 - (C 3 -C 6)环烷基,R 4是基团= CN(CH 3)2,m是0,1,2 ,3或4.本发明还涉及一种制备式(I)化合物的方法,其中X是任选保护的甲酰基,R是本身对于合成的反应条件是惰性的基团 其包括使式(II)化合物(II)与式(III)取代的苯基 - 卤素化合物(III)反应,其中取代基Hal为卤素基团。

    Intermediate steroid compounds
    9.
    发明授权
    Intermediate steroid compounds 失效
    中间类固醇化合物

    公开(公告)号:US5401840A

    公开(公告)日:1995-03-28

    申请号:US105742

    申请日:1993-08-12

    摘要: Novel compounds of the formula ##STR1## wherein either K' is oxygen or a K, a protective group of the oxo of the formula ##STR2## wherein n is 2 or 3, the 17-position dotted line is a bond, R.sub.a and R.sub.b are individually selected from the group consisting of hydrogen, hydroxy, alkyl and alkoxy of 1 to 4 carbon atoms or K' is an oxygen, the 17-position dotted line is an epoxy and R.sub.a and R.sub.b have the meaning indicated above which are useful intermediates for the preparation of hydrocortisone.

    摘要翻译: 新颖的式(Ⅰ)化合物其中K'为氧或K为式(ⅩⅧ)的氧代保护基,其中n为2或3,17位虚线为键,Ra和 Rb分别选自氢原子,羟基,烷基和碳原子数为1〜4的烷氧基或K'为氧,17位虚线为环氧基,Ra和Rb具有上述含义, 用于制备氢化可的松的中间体。

    Supports and their use
    10.
    发明授权
    Supports and their use 失效
    支持及其使用

    公开(公告)号:US4812512A

    公开(公告)日:1989-03-14

    申请号:US878611

    申请日:1986-06-26

    IPC分类号: C07H21/02 C07H21/00 C07H21/04

    CPC分类号: C07H21/00

    摘要: Novel supports useful in solid phase synthesis of oligonucleotides of the formula ##STR1## wherein .circle.P is a material selected from the group consisting of functionalized glass micropellets, silica functionalized by aminoalkyl trialkoxysilane capable of to obtain for ##STR2## Kieselguhr, polytetrafluoroethylene, cellulose and metallic oxides, m is an integer from 1 to 20, A is selected from the group consisting of alkyl of 1 to 20 carbon atoms, saturated cycloalkyl of 3 to 12 carbon atoms, phenyl and 5 to 6 member heterocycles, x and y are an integer from 0 to 20, x.sub.1 is an integer from 1 to 20 and y.sub.1 is an integer from 0 to 10, a process for the preparation of said supports, the use of said supports and intermediates.

    摘要翻译: 新颖的载体可用于固相合成下式的寡核苷酸,其中&cir&P是选自官能化的玻璃微丸,由能够获得 Kieselguhr的氨基烷基三烷氧基硅烷官能化的二氧化硅的材料, 聚四氟乙烯,纤维素和金属氧化物,m是1至20的整数,A选自1至20个碳原子的烷基,3至12个碳原子的饱和环烷基,苯基和5至6个成员杂环,x y为0〜20的整数,x1为1〜20的整数,y1为0〜10的整数,制备所述载体的方法,所述载体和中间体的使用。